The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists

Academic Article
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publication date

  • 2002

abstract

  • Acylated beta-amino acids are described as potent, specific and orally bioavailable antagonists of VLA-4. The initial lead was identified from a combinatorial library. Subsequent optimization using a traditional medicinal chemistry approach led to significant improvement in potency (up to 8-fold) while maintaining good pharmacokinetic properties.